(-)-Isodocarpin (Isodocarpin), a diterpenoid, is a potent melanogenesis inhibitor with an IC50 of 0.19 μM in B16 4A5 cells. (-)-Isodocarpin inhibits the expression of tyrosinase, tyrosine-related protein (TRP)-1, and TRP-2 mRNA[1].
4-Prenyloxyresveratrol, an oxyresveratrol derivative, shows potent tyrosinase inhibitory activity with an IC50 of 0.90 μM[1].
Ferroportin-IN-1 is a ferroportin inhibitor extracted from patent WO2020123850A1 compound 23. Ferroportin-IN-1 can be used for the research of diseases caused by a lack of hepcidin or iron metabolism disorders[1].
Calhex 231 hydrochloride is a CaSR inhibitor via negative allosteric modulation. Calhex 231 hydrochloride blocks Ca2+-induced accumulation of [3H]inositol phosphate with an IC50 of 0.39 μM in HEK293 cells. Calhex 231 hydrochloride has the potential for diabetic cardiomyopathy (DCM) treatment[1][2].
L-Alanine-13C3,15N (L-2-Aminopropionic acid-13C3,15N) is the 13C- and 15N-labeled L-Alanine. L-Alanine is a non-essential amino acid, involved in sugar and acid metabolism, increases immunity, and provides energy for muscle tissue, brain, and central nervous system.
SAR629 is a potent monoglyceride lipase (MGL) covalent inhibitor. SAR629 also inhibits 2-Arachidonoylglycerol (2-AG) degradation[1][2].
Triciribine phosphate (TCN-P) inhibits amidophosphoribosyltransferase by an allosteric mechanism which affects the first committed step of de novo purine biosynthesis. Triciribine phosphate also inhibits IMP dehydrogenase which is the first committed step of guanosine nucleotide synthesis. Tricilibine phosphate does not affect ligase activity[1].
Creatine monohydrate, an endogenous amino acid derivative, plays an important role in cellular energy, especially in muscle and brain[1].
2-Methylbenzaldehyde-13C is the 13C labeled 2-Methylbenzaldehyde[1]. 2-Methylbenzaldehyde is an endogenous metabolite.
1alpha, 25-Dihydroxy VD2-D6 is a deuterated form of vitamin D.
Beauveriolide III is an inhibitor of lipid droplet formation in mouse macrophages[1].
SD-169 is an orally active ATP-competitive inhibitor of p38α MAPK, with an IC50 of 3.2 nM. SD-169 also weakly inhibits p38β MAPK with an IC50 of 122 nM. SD-169 prevents the development and progression of diabetes by inhibiting T cell infiltration and activation[1].
PDE5-IN-4 is a phosphodiesterase 5 inhibitor. PDE5-IN-4 can be used for the research of acute myocardial infarction and damage caused by reperfusion, gastrointestinal diseases, damage caused by diabetes, and liver failure[1].
15-PGDH-IN-1 is a potent and orally active 15-PGDH inhibitior. 15-PGDH-IN-1 has inhibition activity against recombinant human 15-PGDH with an IC50 value of 3 nM. 15-PGDH-IN-1 can be used for the research of tissue repair and regeneration[1].
Lidorestat (IDD-676) is a potent, selective and orally active aldose reductase inhibitor with an IC50 of 5 nM. Lidorestat can be used to treat chronic diabetes complications. Lidorestat also improves nerve conduction and reduces cataract formation[1][2][3].
Cholic acid sodium is a major primary bile acid produced in the liver and usually conjugated with glycine or taurine. It facilitates fat absorption and cholesterol excretion.
Pirinixil is a hypolipidemic agent of low toxicity.
Tienilic acid is a uricosuric diuretic. Tienilic acid possesses certain hepatotoxicity[1][3].
TUG-499 is a selective free fatty acid receptor 1 (FFAR1 or GPR40) (Free Fatty Acid Receptor) agonist with a pEC50 of 7.39. TUG-499 exhibits >100-fold selectivity over the related receptors FFA2, FFA3, and the nuclear receptor PPARγ and other diverse receptors, ion channels, and transporters. TUG-499 can be used for the research of type 2 diabetes[1].
(±)-Abscisic acid is an orally active plant hormone that is present also in animals. (±)-Abscisic acid (ABA) contributes to the regulation of glycemia in mammals[1].
SF0166 is a topically administered αvβ3 integrin antagonist, inhibits integrin-ligand interactions with IC50 of 0.6 nM to 13 nM for human αvβ3, αvβ6, and αvβ8; inhibits cellular adhesion to vitronectin across human, rat, rabbit, and dog cell lines with IC50 of 7.6 pM-76 nM; significantly decreases neovascularization in the oxygen-induced retinopathy mouse models. Other Indication Phase 2 Clinical
Bocidelpar is a modulator of peroxisome proliferator-activated receptor delta (PPAR-δ). Bocidelpar improves mitochondrial biogenesis and function in Duchenne Muscular Dystrophy (DMD) muscle cells (extracted from patent WO2017062468A1, compound 2b)[1].
Zenarestat is a potent and orally active aldose reductase inhibitor. Zenarestat improves diabetic peripheral neuropathy in Zucker diabetic fatty rats[1].
Echistatin, the smallest active RGD protein belonging to the family of disintegrins that are derived from snake venoms, is a potent inhibitor of platelet aggregation. Echistatin is a potent inhibitor of bone resorption in culture. Echistatin is a potent antagonist of αIIbβ3, αvβ3 and α5β1[1][2][3][4].
Cagrilintide is an investigational novel long-acting acylated amylin analogue, acts as nonselective amylin receptors (AMYR) and calcitonin G protein-coupled receptor (CTR) agonist. Cagrilintide induces significant weight loss and reduces food intake. Cagrilintide has the potential for the research of obesity[1][2][3].
NBI-6024, an altered peptide ligand (APL), is an epitope recognized by inflammatory interferon-gamma-producing T helper lymphocytes in type 1 diabetic patients[1][2].
Wilforol A ((-)-Wilforol A), plant metabolite, is a pentacyclic triterpenoid. Wilforol A can be used for the research of various biochemical studies[1].
Retinol, also known as Vitamin A1, has pleiotropic functions including vison, immunity, hematopoiesis, reproduction, cell differentiation/growth, and development.
4,4-Dimethoxy-2-butanone is an endogenous metabolite.
Allopurinol (Zyloprim) is a xanthine oxidase inhibitor with an IC50 of 7.82±0.12 μM.Target: XAOAllopurinol (Zyloprim, and generics) is a drug used primarily to treat hyperuricemia (excess uric acid in blood plasma) and its complications, including chronic gout. It is a xanthine oxidase inhibitor which is administered orally. A common misconception is that allopurinol is metabolized by its target, xanthine oxidase, but this action is principally carried out by Aldehyde oxidase. The active metabolite of allopurinol is oxypurinol, which is also an inhibitor of xanthine oxidase. Allopurinol is almost completely metabolized to oxypurinol within two hours of oral administration, whereas oxypurinol is slowly excreted by the kidneys over 18–30 hours. For this reason, oxypurinol is believed responsible for the majority of allopurinol's effect.Allopurinol is a purine analog; it is a structural isomer of hypoxanthine (a naturally occurring purine in the body) and is an inhibitor of the enzyme xanthine oxidase. In addition to blocking uric acid production, inhibition of xanthine oxidase causes an increase in hypoxanthine and xanthine. While xanthine cannot be converted to purine ribotides, hypoxanthine can be salvaged to the purine ribotides adenosine and guanosine monophosphates. Increased levels of these ribotides may cause feedback inhibition of amidophosphoribosyl transferase, the first and rate-limiting enzyme of purine biosynthesis. Allopurinol, therefore, decreases uric acid formation and may also inhibit purine synthesis.